Abstract
Allylic acetates derived from Baylis-Hillman reaction undergo efficient nucleophilic isomerization with imidazoles and triazoles to provide imidazolylmethyl and triazolylmethyl cinnamates stereoselectively. Antifungal evaluation of these derivatives against Cryptococcus neoformans exhibits good minimum inhibitory concentration values. These compounds exhibit low toxicity in proliferating MCF-7 breast cancer cell line. Structure activity relationship studies indicate that halogenated aromatic derivatives provide better antifungal activity.
Highlights
Due to the advances in modern medicine, overall life expectancy is being greatly extended; the unintended consequence is a large increase in reduced immune system and immunocompromised cancer and organ transplant patients
We initiated the synthesis of BH derived allyl alcohols with various aromatic aldehydes with methyl acrylate in the presence of DABCO
After synthesizing BH derived functionalized imidazoles and triazoles, we evaluated the antifungal efficacy of all these derivatives on a representative fungal species Cryptococcus neoformans
Summary
Due to the advances in modern medicine, overall life expectancy is being greatly extended; the unintended consequence is a large increase in reduced immune system and immunocompromised cancer and organ transplant patients This extension of life expectancy resulted in a lot of opportunistic fungal and bacterial infections often leading to patient mortality. In many developing and poor countries, the usage of amphotericin-B and 5-flucytosine adds a lot of cost burden and treatment may be mainly limited to high-dose azoles. These drugs have many side effects such as hepatotoxicity and myelosuppression [9]. Resistance to azole based therapy has been detected in some Cryptococcus based infections [8] and development of novel and inexpensive azole based therapeutics will be highly beneficial for the treatment of Cryptococcus and other fungal based infections
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